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Long acting injectable formulations

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Title: Long acting injectable formulations.
Abstract: Long acting injectable formulations of macrocyclic lactones comprising a biologically acceptable and biodegradable polyester polymer in a solvent system for use in the field of veterinary medicine, especially for use in combating ecto- and endoparasites in animals. ...

Browse recent Intervet/schering-plough Animal Health patents - Kenilworth, NJ, US
Inventors: Carolina Nunes Costa Corgozinho, Karla de Melo Lima, Jose Maciel Junior Rodriques, Peter Andrew O'Neill
USPTO Applicaton #: #20110039794 - Class: 514 28 (USPTO) - 02/17/11 - Class 514 
Drug, Bio-affecting And Body Treating Compositions > Designated Organic Active Ingredient Containing (doai) >O-glycoside >Oxygen Of The Saccharide Radical Bonded Directly To A Nonsaccharide Hetero Ring Or A Polycyclo Ring System Which Contains A Nonsaccharide Hetero Ring >The Hetero Ring Has 8 Or More Ring Carbons

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The Patent Description & Claims data below is from USPTO Patent Application 20110039794, Long acting injectable formulations.

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This application relates to long acting injectable formulations of macrocyclic lactones comprising a biodegradable polyester polymer in a solvent or solvent system for use in the field of veterinary medicine, especially for use in combating ecto- and endoparasites in animals.


Ecto- and Endo-Parasites of Animals

A number of pests and parasites can infest or infect livestock animals and also companion animals such as cats, dogs and horses. These pests and parasites are of great nuisance to both the animals and their owners.

Virtually all livestock and companion animals are affected by ectoparasites, i.e. arthropods which are injurious to, or spread or act as vectors of diseases in man and livestock and companion animals. Important arthropod parasites—ectoparasites (insect and acarid pests) are described below in more detail.

Biting insects include, e.g., migrating diperous larvae as Hypoderma sp. in cattle, Gastrophilus in horses, and Cuterebra sp. in rodents, as well as biting flies and mosquitoes spp of all types. For example, bloodsucking adult flies include, e.g., the horn fly or Haematobia irritans, the horse fly or Tabanus spp., the stable fly or Stomoxys calcitrans, the black fly or Simulium spp., the deer fly or Chrysops spp., the louse fly or Melophagus ovinus, the tsetse fly or Glossina spp. Parasitic fly maggots include, e.g., the bot fly (Oestrus ovis and Cuterebra spp.), the blow fly or Phaenicia spp., the screwworm or Cochliomyia hominivorax, the cattle grub or Hypoderma spp., and the fleeceworm. Mosquitoes, include, for example, Culex spp., Anopheles spp., and Aedes spp.

Mites include Mesostigmata spp. e.g., mesostigmatids such as the chicken mite, Dermanyssus gallinae; itch or scab mites such as Sarcoptidae spp. for example, Sarcoptes scabiei; mange mites such as Psoroptidae spp. including Chorioptes bovis and Psoroptes ovis; chiggers e.g., Trombiculidae spp.

Ticks include, e.g., soft-bodied ticks including Argasidae spp. for example Argas spp. and Ornithodoros spp.; hard-bodied ticks including Ixodidae spp., for example Ixodes ricinus, Rhipicephalus sanguineus, Haemaphysalis spp, Dermacentor reticulates, Dermacentor variabilis, Amblyomma americanum and Boophilus spp.

Lice include, e.g., sucking lice, e.g., Menopon spp. and Bovicola spp.; biting lice, e.g., Haematopinus spp., Linognathus spp. and Solenopotes spp.

Fleas include, e.g., Ctenocephalides spp., such as dog flea (Ctenocephalides canis) and cat flea (Ctenocephalides fells); Xenopsylla spp. such as oriental rat flea (Xenopsylla cheopis); and Pulex spp. such as human flea (Pulex irritans).

True bugs include, e.g., Cimicidae or e.g., the common bed bug (Cimex lectularius); Triatominae spp. including triatomid bugs also known as kissing bugs; for example Rhodnius prolixus and Triatoma spp.

Important endoparasites of animal hosts are parasitic worms known as helminths. Among the helminths, the group of worms described as nematodes causes widespread and often serious infection in various species of animals. The parasitic infections known as helminthiases lead to anemia, malnutrition, weakness, weight loss, severe damage to the walls of the intestinal tract and other tissues and organs, and, if left untreated, may result in death of the infected host. Helminthiasis is a prevalent and serious economic problem in domesticated animals such as swine, sheep, horses, cattle, goats, dogs, cats and poultry.

The most common genera of nematodes infecting the animals referred to above are Haemonchus, Trichostrongylus, Ostertagia, Nematodirus, Cooperia, Ascaris, Bunostomum, Oesophagostomum, Chabertia, Trichuris, Strongylus, Trichonema, Dictyocaulus, Capillaria, Heterakis, Toxocara, Ascaridis, Oxyuris, Ancylostoma, Uncinaria, Toxascaris and Parascaris. Certain of these, such as Nematodirus, Cooperia and Oesophagostomum, attack primarily the intestinal tract. Others, such as Haemonchus and Ostertagia, are more prevalent in the stomach. Others, such as Dictyocaulus, are found in the lungs. Still other parasites may be located in other tissues and organs of the body such as the heart and blood vessels, subcutaneous and lymphatic tissue, and the like.

Macrocyclic Lactones

The macrocyclic lactones, i.e. avermectin and milbemycin series of compounds are potent endo- and ectoparasitic agents. The compounds which belong to this series are either natural products or are semi-synthetic derivatives thereof. The structure of these two series of compounds are closely related and they both share a complex 1,6-membered macrocyclic lactone ring; however, the milbemycins do not contain the disaccharide substituent in the 1,3-position of the lactone ring.

In a preferred embodiment of the invention, the macrocyclic lactones e.g. avermectins, milbemycins and derivatives thereof are selected from the group which includes but is not limited to, abamectin, doramectin, emamectin, eprinomectin, ivermectin, and selamectin (avermectin and derivatives thereof), milbemycin D, milbemycin oxime, lepimectin, and moxidectin (milbemycin and derivatives thereof) and mixtures thereof.

One particularly contemplated macrocyclic lactone parasiticide is ivermectin. Ivermectin is a semi-synthetic derivative of avermectin, and is generally produced as a mixture of at least 80% 22,23-dihydroavermectin B1a and less than 20% 22,23-dihydroavermectin B1b. Ivermectin is disclosed in U.S. Pat. No. 4,199,569. Ivermectin has been used as an antiparasitic agent to treat various parasitic diseases since the mid-1980\'s.

Other macrocyclic lactone parasiticides include, for example: Abamectin. This compound is, for example, identified as avermectin B1a/B1b in U.S. Pat. No. 4,310,519. Abamectin contains at least 80% of avermectin B1a, and not more than 20% of avermectin B1b. Doramectin. This compound is known as 25-cyclohexyl-avermectin B1. Its structure and preparation are discussed in, for example, U.S. Pat. No. 5,089,480. Emamectin. This compound also is known as 4″-deoxy-4″-epi-methylaminoavermectin B1. Its preparation is discussed in, for example, U.S. Pat. Nos. 5,288,710 and 5,399,717. Eprinomectin. This compound is known as 4″-epi-acetylamino-4″-deoxy-avermectin B1. It was developed for use in all cattle classes and age groups. Selamectin. This compound also is known as 25-cyclohexyl-25-de(1-methyl propyl)-5-deoxy-22,23-dihydro-5-(hydroxyimino)-avermectin B1 monosaccharide. Milbemycin. This compound also is known as B41. It is isolated from the fermentation broth of a Milbemycin-producing strain of Streptomyces. The microorganism, fermentation conditions, and isolation procedures are discussed in, for example, U.S. Pat. Nos. 3,950,360 and 3,984,564. Moxidectin. This compound is discussed in, for example, U.S. Pat. No. 4,916,154. Lepimectin is a chemically modified milbemycin macrolide (6R,13R,25R)-5-O-demethyl-28-deoxy-6,28-epoxy-13-[(Z)-[(methoxyimino)phenylacetyl]oxy]-25-methylmilbemycin B mixture with (6R,13R,25R)-5-O-demethyl-28-deoxy-6,28-epoxy-25-ethyl-13-[(Z)-[(methoxyimino)phenylacetyl]oxy]milbemycin B.

While the individual macrocyclic lactones are well-known in the art, there have been difficulties in the art to provide for a viable, easy to use, long acting injectable formulation containing these endectoparasitic agents.

Controlled-Release Technology

In the field of human and veterinary medicine many advantages are offered by controlled-, and especially prolonged release technology. First, controlled release of a pharmaceutical agent allows less frequent dosing and thus minimizes handling of animals. Further, controlled release treatment results in more efficient drug utilization. Further, less of the compound remains as a residue.

In the prior art many different concepts of prolonged release of injectable pharmaceutical compositions in animals have been described, e.g. use of low water soluble forms or complexes of active ingredients, use of liposome, microsphere and liposphere formulations, polymer formulations, oil based formulations, gel formulations etc.

Such concepts have been reviewed e.g. in Medlicott et al “Sustained release veterinary parenteral products”, Advanced Drug Delivery Reviews 56; (2004), p. 1345-1365, in Winzenburg et al” Biodegradable polymers and their potential use in parenteral veterinary drug delivery systems“, Advanced Drug Delivery Reviews 56; (2004), p. 1453-1466, in Matschke et al “Sustained-release injectables formed in situ and their potential use for veterinary products”, Journal of Controlled Release 85; (2002), p. 1-15 and in Packhaeuser et al “In situ forming parenteral drug delivery systems: an overview”, European Journal of Pharmaceutics and Biopharmaceutics 58; (2004), p. 445-455.

Despite these advantages, however, few prolonged release formulations for parenteral administration have been developed for commercial use in veterinary medicine.

Hence, there is still a need in the art for long acting formulations for prolonged release which are suitable for injection and which have long term shelf stability. In addition, an ideal injectable formulation would have a long acting effect that would have a season long effect during the breeding period for livestock mammals such as cattle, sheep, goats and pigs or minimize the number of injections when applying to companion mammals such as dogs, cats and horses.



In view of the above-described state of the art, the objects of the invention are to provide a long acting injectable antiparasitic composition that combines the advantages of minimal repetitive administration, efficient drug utilization, and minimal handling.

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stats Patent Info
Application #
US 20110039794 A1
Publish Date
Document #
File Date
514 28
Other USPTO Classes
International Class

Solvent System

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